Correlation between microstructure and bioequivalence in Anti-HIV Drug

Solid-state characteristics of drugs can impact their dissolution behaviour and, as a consequence, their bioavailability, affecting, thus, the bioequivalence of generic drugs. Bioequivalence of a poor-soluble drug, such as the anti-HIV Efavirenz, needs to be assessed by studying polymorphism particle size distributions and microstructure.
 

Structural and microstructural information of several batches of Efavirenz were investigated through Whole Powder Pattern Modelling (WPPM) of synchrotron radiation X-ray powder diffraction data. Results showed the correlation between crystalline domain size distributions and bioequivalence studies, proving that deeper knowledge of the crystalline domain size distribution should be obtained during pharmaceutical developments, in order to gain bioequivalence success.